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ChEMBL ligand: CHEMBL11298 (L-(-)-serine, L-serine, NSC-118365, Serine) |
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DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
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Acetylcholinesterase in Electrophorus electricus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4078] [UniProtKB: O42275] | ||||||||
ChEMBL | Inhibition of Electrophorus electricus acetylcholinesterase using acetylthiocholine iodide as substrate preincubated for 20 mins followed by substrate addition measured for 30 mins by Ellman's method | B | 7.82 | pIC50 | 15 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2654-2656 [PMID:25980913] |
Amino acid transporter in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL3562161] [UniProtKB: Q9Z1J7] | ||||||||
ChEMBL | Inhibition of ASCT2 mediated [3H]-L-serine uptake in rat hippocampal astrocytes after 5 mins by beta counting analysis | B | 4.03 | pIC50 | 94000 | nM | IC50 | US-8741955-B2. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of central nervous system disorders (2014) |
ChEMBL | Inhibition of ASCT2 mediated [3H]-D-serine uptake in rat hippocampal astrocytes | B | 4.24 | pIC50 | 57900 | nM | IC50 | US-8741955-B2. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of central nervous system disorders (2014) |
Asc-type amino acid transporter 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL4105976] [GtoPdb: 901] [UniProtKB: P63116] | ||||||||
ChEMBL | Inhibition of asc-1 mediated [3H]-D-serine uptake in P2 fraction of rat forebrain synaptosomes after 4 mins by beta scintillation counting | B | 5.02 | pIC50 | 9600 | nM | IC50 | US-8741955-B2. D-serine transporter inhibitors as pharmaceutical compositions for the treatment of central nervous system disorders (2014) |
Cholinesterase in Equus caballus (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL5763] [UniProtKB: P81908] | ||||||||
ChEMBL | Inhibition of equine serum butyrylcholinesterase using butyrylthiocholineidioide as substrate preincubated for 20 mins followed by substrate addition measured for 30 mins by Ellman's method | B | 7.8 | pIC50 | 16 | nM | IC50 | Bioorg Med Chem Lett (2015) 25: 2654-2656 [PMID:25980913] |
Gamma-glutamyltranspeptidase 1 in Rat (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2943] [UniProtKB: P07314] | ||||||||
ChEMBL | Inhibition of Rattus norvegicus Wistar (rat) rat Gamma-glutamyltranspeptidase using L-gamma-glutamyl-p-nitroanilide as substrate incubated for 15 min prior to substrate addition by spectrophotometric analysis | B | 4.3 | pKi | 50000 | nM | Ki | Med Chem Res (2004) 13: 707-723 |
Proton-coupled Amino acid Transporter 1/Proton-coupled amino acid transporter 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL1914279] [GtoPdb: 1161] [UniProtKB: Q7Z2H8] | ||||||||
ChEMBL | Inhibition of human PAT1-mediated L-[3H]proline uptake in human Caco2 cells after 10 mins by liquid scintillation counting | B | 1.54 | pKi | -1.54 | mM | pKi | Bioorg Med Chem (2011) 19: 6409-6418 [PMID:21955456] |
GPRC6 receptor in Human [GtoPdb: 55] [UniProtKB: Q5T6X5] | ||||||||
GtoPdb | - | - | 3.2 | pEC50 | - | - | - | Mol Pharmacol (2005) 67: 589-97 [PMID:15576628] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]